【结 构 式】 |
【药物名称】Cerebrocrast, IOS-1.1212 【化学名称】4-[2-(Difluoromethoxy)phenyl]-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylic acid di(2-propoxyethyl) diester 【CA登记号】108863-62-3 【 分 子 式 】C26H35F2NO7 【 分 子 量 】511.56815 |
【开发单位】Latvian Institute of Organic Synthesis (Originator) 【药理作用】Antidiabetic Drugs, Cerebrovascular Diseases, Treatment of, ENDOCRINE DRUGS, NEUROLOGIC DRUGS, Stroke, Treatment of, Calcium Channel Blockers |
合成路线1
Cerebrocrast is prepared in Hantzsch-type reaction from 2-(propoxy)ethyl acetoacetate (III), 2-(difluoromethoxy)benzaldehyde and ammonia, or from 2-(propoxy)ethyl beta-aminocrotonate (IV) and 2-(difluoromethoxy)benzaldehyde. The necessary raw material, 2-(propoxy)ethyl acetoacetate (III), is prepared from 2-(propoxy)ethanole (II) by acetoacetylation with diketene (I).
【1】 Klusa, V.; Cerebrocrast. Drugs Fut 1995, 20, 2, 135. |
【2】 Makarova, N.V.; Biseniex, E.A.; Uldrikis, Y.R.; Dubur, G.Y.; Veveris, M.M.; Kimenis, A.A. (Latvian Institute of Organic Synthesis); Alkoxy- and phenoxy-alkyl esters of 2,6-dimethyl-4-(2-difluoromethoxyphenyl)-1,4-dihydropyridine-3,5-dicarboxylic acid. FR 2587701 . |
【3】 Dubur, G.J.; Veveris, M.M.; Weinheimer, G.; Bisenieks, E.A.; Makarova, N.V.; Kimenis, A.A.; Uldrikis, J.R.; Lukevics, E.J.; Dooley, D.; Osswald, H.; Synthesis and selective vasodilating properties of esters of 2,6-dimethyl-4-(2-difluoromethoxyphenyl)-1,4-dihydropyridine-3,4-dicarboxylic acid. Arzneim-Forsch Drug Res 1989, 39, 10, 1185-9. |